Substituted 4,5,6,7-tetrahydroindoles and their fused derivatives. Synthesis and cytotoxic activity towards tumor and normal human cell lines

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Date

2013

Journal Title

Journal ISSN

Volume Title

Type

Article

Publisher

SPRINGER

Series Info

CHEMISTRY OF HETEROCYCLIC COMPOUNDS;Volume: 49 Issue: 8 Pages: 1212-1223

Abstract

This work has been carried out to explore the reaction of 2-cyanoacetohydrazide with cyclohexanone to form 4,5,6,7-tetrahydroindole derivatives. 2-Hydroxy-4,5,6,7-tetrahydro-1H-indole-3-carbonitrile was used as the starting material for a series of novel heterocyclic products containing fused oxazine, pyran, pyrazole, pyridazine, and thiophene rings. The antitumor activity evaluation of the newly synthesized compounds against three human tumor cells lines, breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460), and CNS cancer (SF-268), and with normal fibroblast cells (WI 38) showed that some of these compounds exhibit much higher inhibitory effects towards the three tumor cell lines than the reference drug doxorubicin while being minimally active towards normal cells.

Description

Accession Number: WOS:000326375500016

Keywords

University of DRUG DISCOVERY, Indoles, Pyrans, Antitumor activity

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